Prasugrel Active Metabolite
Active Metabolite of Prasugrelas reference standard for the analytical determination of prasugrel in bioavailability and bioequivalence studies
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After oral administration prasugrel is rapidly metabolized by esterases to the thiolactone R-95913, which is then oxidatively metabolized to the active metabolite R-138727. The parent compound prasugrel is not detectable in human plasma after oral administration. All pharmacokinetic investi-gations in humans relevant for the approval of prasugrel are therefore performed by analysing R-138727, the active metabolite. R-138727 is highly unstable in plasma and must be derivatized immediately after blood sampling with 2-bromo-3'-methoxyacetophenone. |
HELM offers |
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| - trans-R 138727MP: | |
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Helm offers the derivatized trans-R-138727MP and the deuterated compound R-138727MP-d3. |
| - trans-R-138727MP-d3: | |
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The determination of R-138727 in plasma is described in several research articles, e.g. N. A. Farid et.al, Rapid Commun. Mass Spectrom. 2007, 21, 169 – 179. |
Helm's compounds R-138727MP and R 138727MP d3 were used as standards to analyse the plasma samples of a comparative bioavailability study with two Prasugrel 10 mg formulations.
Mean R-138727 plasma concentrations after fasting administration of a prasugrel test formulation vs. Efient
For further information please contact:
Mr. Axel Bourjau
A. Bourjau@helmag.com
Phone: 0049-40-2375- 1004